LY-487,379

LY-487,379
Clinical data
ATC code	none;
Identifiers
	IUPAC name N-(4-(2-methoxyphenoxy)phenyl)- N-(2,2,2-trifluoroethylsulfonyl)pyrid- 3-ylmethylamine;
PubChem CID	9825084;
IUPHAR/BPS	1402;
ChemSpider	8000831 ;
ChEMBL	ChEMBL108939 ;
CompTox Dashboard (EPA)	DTXSID10431366 ;
Chemical and physical data
Formula	C21H19F3N2O4S
Molar mass	452.446 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c3ncccc3CN(S(=O)(=O)CC(F)(F)F)c2ccc(cc2)Oc1ccccc1OC;
	InChI InChI=1S/C21H19F3N2O4S/c1-29-19-6-2-3-7-20(19)30-18-10-8-17(9-11-18)26(14-16-5-4-12-25-13-16)31(27,28)15-21(22,23)24/h2-13H,14-15H2,1H3 ; Key:ALMACYDZFBMGOR-UHFFFAOYSA-N ;
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LY-487,379 is a drug used in scientific research that acts as a selective positive allosteric modulator for the metabotropic glutamate receptor group II subtype mGluR₂.[1] It is used to study the structure and function of this receptor subtype,[2][3] and LY-487,379 along with various other mGluR_2/3 agonists and positive modulators are being investigated as possible antipsychotic and anxiolytic drugs.[4][5][6][7][8]

References

Johnson, M. P.; Baez, M.; Jagdmann, G. E.; Britton, T. C.; Large, T. H.; Callagaro, D. O.; Tizzano, J. P.; Monn, J. A.; Schoepp, D. D. (2003). "Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity ofN-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine". Journal of Medicinal Chemistry. 46 (15): 3189–3192. doi:10.1021/jm034015u. PMID 12852748.
Schaffhauser, H.; Rowe, B. A.; Morales, S.; Chavez-noriega, L. E.; Yin, R.; Jachec, C.; Rao, S. P.; Bain, G.; et al. (2003). "Pharmacological Characterization and Identification of Amino Acids Involved in the Positive Modulation of Metabotropic Glutamate Receptor Subtype 2". Molecular Pharmacology. 64 (4): 798–810. doi:10.1124/mol.64.4.798. PMID 14500736.
Poisik, O.; Raju, D. V.; Verreault, M.; Rodriguez, A.; Abeniyi, O. A.; Conn, P. J.; Smith, Y. (2005). "Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus". Neuropharmacology. 49: 57–69. doi:10.1016/j.neuropharm.2005.03.006. PMID 15993439.
Galici, R.; Echemendia, N. G.; Rodriguez, A. L.; Conn, P. J. (2005). "A Selective Allosteric Potentiator of Metabotropic Glutamate (mGlu) 2 Receptors Has Effects Similar to an Orthosteric mGlu2/3 Receptor Agonist in Mouse Models Predictive of Antipsychotic Activity". Journal of Pharmacology and Experimental Therapeutics. 315 (3): 1181–7. doi:10.1124/jpet.105.091074. PMID 16123306.
Marino; Conn, P. (2006). "Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors". Current Opinion in Pharmacology. 6 (1): 98–102. doi:10.1016/j.coph.2005.09.006. PMID 16368268.
Harich; Gross, G.; Bespalov, A. (2007). "Stimulation of the metabotropic glutamate 2/3 receptor attenuates social novelty discrimination deficits induced by neonatal phencyclidine treatment". Psychopharmacology. 192 (4): 511–519. doi:10.1007/s00213-007-0742-y. PMID 17318501.
Conn, P. J.; Jones, C. K. (2009). "Promise of mGluR2/3 activators in psychiatry". Neuropsychopharmacology. 34 (1): 248–249. doi:10.1038/npp.2008.156. PMC 2907744. PMID 19079073.
Hermes, M. L. H. J.; Renaud, L. P. (2010). "Postsynaptic and Presynaptic Group II Metabotropic Glutamate Receptor Activation Reduces Neuronal Excitability in Rat Midline Paraventricular Thalamic Nucleus". Journal of Pharmacology and Experimental Therapeutics. 336 (3): 840–849. doi:10.1124/jpet.110.176149. PMID 21139059.

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[1] Johnson, M. P.; Baez, M.; Jagdmann, G. E.; Britton, T. C.; Large, T. H.; Callagaro, D. O.; Tizzano, J. P.; Monn, J. A.; Schoepp, D. D. (2003). "Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity ofN-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine". Journal of Medicinal Chemistry. 46 (15): 3189–3192. doi:10.1021/jm034015u. PMID 12852748.

[2] Schaffhauser, H.; Rowe, B. A.; Morales, S.; Chavez-noriega, L. E.; Yin, R.; Jachec, C.; Rao, S. P.; Bain, G.; et al. (2003). "Pharmacological Characterization and Identification of Amino Acids Involved in the Positive Modulation of Metabotropic Glutamate Receptor Subtype 2". Molecular Pharmacology. 64 (4): 798–810. doi:10.1124/mol.64.4.798. PMID 14500736.

[3] Poisik, O.; Raju, D. V.; Verreault, M.; Rodriguez, A.; Abeniyi, O. A.; Conn, P. J.; Smith, Y. (2005). "Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus". Neuropharmacology. 49: 57–69. doi:10.1016/j.neuropharm.2005.03.006. PMID 15993439.

[4] Galici, R.; Echemendia, N. G.; Rodriguez, A. L.; Conn, P. J. (2005). "A Selective Allosteric Potentiator of Metabotropic Glutamate (mGlu) 2 Receptors Has Effects Similar to an Orthosteric mGlu2/3 Receptor Agonist in Mouse Models Predictive of Antipsychotic Activity". Journal of Pharmacology and Experimental Therapeutics. 315 (3): 1181–7. doi:10.1124/jpet.105.091074. PMID 16123306.

[5] Marino; Conn, P. (2006). "Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors". Current Opinion in Pharmacology. 6 (1): 98–102. doi:10.1016/j.coph.2005.09.006. PMID 16368268.

[6] Harich; Gross, G.; Bespalov, A. (2007). "Stimulation of the metabotropic glutamate 2/3 receptor attenuates social novelty discrimination deficits induced by neonatal phencyclidine treatment". Psychopharmacology. 192 (4): 511–519. doi:10.1007/s00213-007-0742-y. PMID 17318501.

[7] Conn, P. J.; Jones, C. K. (2009). "Promise of mGluR2/3 activators in psychiatry". Neuropsychopharmacology. 34 (1): 248–249. doi:10.1038/npp.2008.156. PMC 2907744. PMID 19079073.

[8] Hermes, M. L. H. J.; Renaud, L. P. (2010). "Postsynaptic and Presynaptic Group II Metabotropic Glutamate Receptor Activation Reduces Neuronal Excitability in Rat Midline Paraventricular Thalamic Nucleus". Journal of Pharmacology and Experimental Therapeutics. 336 (3): 840–849. doi:10.1124/jpet.110.176149. PMID 21139059.

LY-487,379

See also

References